Amiodarone (NSC 85442) HCl

Catalog No.S1979

For research use only.

Amiodarone (NSC 85442) HCl is a sodium/potassium-ATPase inhibitor and an autophagy activator, used to treat various types of cardiac dysrhythmias.

Amiodarone (NSC 85442) HCl Chemical Structure

CAS No. 19774-82-4

Selleck's Amiodarone (NSC 85442) HCl has been cited by 8 Publications

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Purity & Quality Control

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Biological Activity

Description Amiodarone (NSC 85442) HCl is a sodium/potassium-ATPase inhibitor and an autophagy activator, used to treat various types of cardiac dysrhythmias.
Targets
Potassium channel [1]
In vitro

Amiodarone possesses an inhibitory effect on the fast sodium channel as well as on the slow calcium channel. Amiodarone also has non-competitive antisympathetic effects, and modulates thyroid function and phospholipid metabolism. Amiodarone penetrates deeply into the lipid matrix of the membrane, and is released from cardiac tissues very slowly when washed out. Amiodarone (44–88 μM) depresses Vmax of guinea pig papillary muscle without affecting the resting membrane potential, and that this Vmax inhibition is enhanced in a frequency- or use-dependent manner like Class I antiarrhythmic drugs. Amiodarone (50–88 μM) is also found to suppress the depolarization-induced spontaneous action potentials (abnormal automaticity) in ventricular muscles and in Purkinje fibers. [1]

In vivo Amiodarone (1.25–25 mg/kg) results in a decrease in sinus rate, a prolongation of effective and functional refractory periods of the atrioventricular node, and a frequency-dependent conduction delay in the atrioventricular node and in the ventricle of anesthetized dogs. Amiodarone (50 mg/kg/day, i.p. for 3–4 weeks) results in significant decreases in the current density of iK and ito in ventricular cells without affecting iCa and iK1 densities in rabbit. Amiodarone (AM) inhibits intracellular conversion from thyroxine (T4) to triiodothyronine (T3) via 5′-deiodination (5′DI) without affecting intracellular conversion from T4 to reverse T3 (rT3). [1]

Protocol (from reference)

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.

3mg/mL

Chemical Information

Molecular Weight 681.77
Formula

C25H29I2NO3.HCl

CAS No. 19774-82-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCCCC1=C(C2=CC=CC=C2O1)C(=O)C3=CC(=C(C(=C3)I)OCCN(CC)CC)I.Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05287191 Recruiting Drug: Magnesium sulfate and then Digoxin|Drug: Amiodarone Atrial Fibrillation New Onset Sunnybrook Health Sciences Centre|Sunnybrook Research Institute January 5 2022 Phase 3
NCT05171985 Not yet recruiting Procedure: Dexmedetomidine sedation COVID-19 Pneumonia|Atrial Fibrillation Tanta University January 2022 Not Applicable
NCT03991754 Unknown status Procedure: transcatheter aortic valve implantation Atrial Fibrillation New Onset Luis Nombela Franco|Hospital San Carlos Madrid June 30 2019 Phase 3
NCT03842020 Completed Other: Blood pharmacokinetic samples Heart Rhythm Disorder Assistance Publique - Hôpitaux de Paris|URC-CIC Paris Descartes Necker Cochin February 13 2019 Not Applicable
NCT03919097 Completed Other: Medical Data extraction Flutter José Castro|Brugmann University Hospital January 8 2019 --

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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